A New Hypoxia Inducible Factor-2 Inhibitory Pyrrolinone Alkaloid from Roots and Stems of Piper sarmentosum

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概要

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• A new trimethoxycinnamoyl-2-pyrrolinone alkaloid, langkamide (1), along with the known compounds piplartine (2) and 3,4,5-trimethoxycinnamic acid (3) were isolated from the roots and stems of the shrub Piper sarmentosum ROXB. The structures were established by spectroscopic analyses and comparison of their spectral data with values reported in the literature. The compounds were tested for their ability to modulate hypoxia inducible factor-2 (HIF-2) transcription activity and all three showed HIF-2 inhibitory activity with EC50 values of 14.0, 4.8, and 60.6 μM, respectively, for compounds 1, 2, and 3.

著者

• McMahon James

  Molecular Targets Laboratory, Center for Cancer Research

• Bokesch Heidi

  SAIC-Frederick, Inc.

• Gardella Roberta

  SAIC-Frederick, Inc.

• Rabe Daniel

  Urologic Oncology Branch, Center for Cancer Research, National Cancer Institute, U.S.A

• Bottaro Donald

  Urologic Oncology Branch, Center for Cancer Research, National Cancer Institute, U.S.A

• Linehan William

  Urologic Oncology Branch, Center for Cancer Research, National Cancer Institute, U.S.A

• McKee Tawnya

  Molecular Targets Laboratory, Center for Cancer Research

• McMahon James

  Molecular Targets Development Program, NCl

関連論文

• A New Hypoxia Inducible Factor-2 Inhibitory Pyrrolinone Alkaloid from Roots and Stems of Piper sarmentosum
• P-42 ABCG2多剤耐性トランスポーター阻害剤botryllamidesに関する研究(ポスター発表の部)

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